[CAS NO. 176199-48-7]??Eglumegad
PRODUCTS SPECIFICATIONS [176199-48-7]
DESCRIPTION [176199-48-7]
Overview
| MDL | MFCD04113018 |
|---|---|
| Molecular Weight | 185.18 |
| Molecular Formula | C8H11NO4 |
| SMILES | OC([C@]1([C@]2([H])[C@@H](C(O)=O)[C@]2([H])CC1)N)=O |
2 Publications Citing Use of MCE
Summary
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC 50 s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
IC50 & Target
|
mGluR2R 5 nM (IC 50 ) |
mGluR3R 24 nM (IC 50 ) |
In Vitro
Eglumegad (LY354740) down-regulates spots 1014, 1822 (hypoxia up-regulated protein 1), 4513 (an isoform of protein disulfide isomerase 3), 6204, 6312, 7306 (26S proteasome non-ATPase regulatory subunit 7) and protein spots 1013 and 6005 (destrin), and up-regulates spot 6507 (collapsin response mediator protein 1) in mouse cortical neurons [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) has no effect on spatial working memory performance in Gria1 ?/? or WT mice, and it has no effect on rewarded alternation testing with a short inter-trial interval in Gria1 ?/? and WT mice at concentration of 30 mg/kg. Eglumegad (LY354740) (15 or 30 mg/kg, i.p.) reduces spontaneous locomotor activity in wild-type and Gria1 ?/? mice [1] . Eglumegad (LY354740) (15 mg/kg, i.p.) dreases novelty-induced hyperlocomotion in naive GluA1-KO and pre-handled GluA1-KO males, but not in females. Eglumegad (LY354740) (15 mg/kg, i.p.) significantly reduces the increased c-Fos expression of GluA1-KO males to the level of WT males, but not in of females [3] . Eglumegad (LY354740) (10 mg/kg, i.p.) attenuates the immobilization stress-induced increase in BDNF mRNA expression in the rat mPFC [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
H 2 O : 6.33 mg/mL ( 34.18 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.4002 mL | 27.0008 mL | 54.0015 mL |
| 5 mM | 1.0800 mL | 5.4002 mL | 10.8003 mL |
| 10 mM | 0.5400 mL | 2.7001 mL | 5.4002 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 2.86 mg/mL (15.44 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
References
- [1] Boerner T, et al. The group II metabotropic glutamate receptor agonist LY354740 and the D2 receptor antagonist haloperidol reduce locomotor hyperactivity but fail to rescue spatial working memory in GluA1 knockout mice. Eur J Neurosci. 2017 Apr;45(7):912-
- [2] Orlando R, et al. Levels of the Rab GDP dissociation inhibitor (GDI) are altered in the prenatal restrain stress mouse model of schizophrenia and are differentially regulated by the mGlu2/3 receptor agonists, LY379268 and LY354740. Neuropharmacology. 2014
- [3] Procaccini C, et al. Reversal of novelty-induced hyperlocomotion and hippocampal c-Fos expression in GluA1 knockout male mice by the mGluR2/3 agonist LY354740. Neuroscience. 2013 Oct 10;250:189-200
- [4] Lee Y, et al. The mGlu2/3 receptor agonist LY354740 suppresses immobilization stress-induced increase in rat prefrontal cortical BDNF mRNA expression. Neurosci Lett. 2006 May 8;398(3):328-32.
Synonyms